As well as its needed effects, theophylline may cause unwanted side effects that require medical attention.

If any of the following side effects occur while taking theophylline, check with your doctor immediately:

Incidence not known

Chest pain or discomfort

dizziness

fainting

fast, slow, or irregular heartbeat

increase in urine volume

lightheadedness

persistent vomiting

pounding or rapid pulse

seizures

shakiness

If any of the following symptoms of overdose occur while taking theophylline, get emergency help immediately:

Symptoms of overdose

Abdominal or stomach pain

blurred vision

confusion

confusion about identity, place, and time

dark-colored urine

decrease in frequency of urination

decreased urine

diarrhea

difficulty in passing urine (dribbling)

dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position

dry mouth

fast, pounding, or irregular heartbeat or pulse

fever

increased thirst

irregular heartbeat

loss of appetite

mood changes

muscle cramps or spasms

muscle pain or stiffness

nausea or vomiting

nervousness

numbness or tingling in the hands, feet, or lips

pain or discomfort in the arms, jaw, back, or neck

painful urination

shakiness in the legs, arms, hands, or feet

shortness of breath

sweating

unusual tiredness or weakness

vomiting of blood or material that looks like coffee grounds

Some theophylline side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them:

Incidence not known

Headache

irritability

restlessness

sleeplessness

trouble sleeping

unable to sleep

For Healthcare Professionals

General

The majority of side effects have been dependent on the serum concentration. Generally, serum concentrations of theophylline ranging from 10 to 20 mcg/mL are considered therapeutic, and serum concentrations greater than 20 mcg/mL are associated with greater toxicity.[Ref]

There are several factors which may predispose a patient to higher serum concentrations and, thus, toxicity. These factors may include increased age, concomitant drugs which reduce the clearance of theophylline, hypothyroidism, congestive heart failure, liver disease, renal failure, and alterations in smoking habits. One series of patients with theophylline intoxication had recent upper respiratory tract infections.

The nature of acute toxicity of theophylline differs from chronic toxicity. Acute overdose is associated with higher theophylline concentrations and younger patients. In acute overdose the severity of toxicity is correlated with peak serum concentrations. Chronic overdosage is seen more commonly in older patients, and severe toxicity may occur with serum concentrations which are much lower than those seen in severe acute toxicity. In these patients, age is a predictor of severe toxicity.[Ref]

Gastrointestinal

Gastrointestinal side effects have included anorexia, nausea, vomiting, and abdominal pain. Theophylline may also cause locally-mediated gastrointestinal upset.[Ref]

Nervous system

Nervous system side effects have included generalized seizures, most commonly in patients with elevated serum concentrations, although seizures have occurred at therapeutic concentrations. Theophylline may also cause nervousness and tremor at therapeutic dosages, which become worse as serum concentrations increase.[Ref]

The mechanism of theophylline-induced seizures has not been determined. Seizures are generally focal with secondary generalization. Permanent neurologic deficits have been reported and morbidity may be high, especially in the elderly, patients with severe underlying disease, and patients with prolonged, uncontrolled seizure activity. The onset of seizures is not always preceded by less severe symptoms of theophylline toxicity. Patients with an abnormal neurologic history, including a history of seizures, cerebral infarct, or head trauma, may be predisposed to seizure activity. If theophylline is used in these types of patients, serum concentrations should be monitored closely and maintained in the low, therapeutic range.[Ref]

Cardiovascular

Cardiovascular side effects have included increases in heart rate which have progressed to supraventricular tachycardia or ventricular tachycardia. Patients with a history of arrhythmias may be predisposed to this effect. Hypotension has occurred with rapid intravenous administration.[Ref]

Theophylline serum concentrations have been a significant predictor of arrhythmias. One study reported multifocal atrial tachycardia in 8% and 16% of patients with a serum concentration between 10 and 20 mcg/mL and greater than 20 mcg/mL, respectively. The onset of serious arrhythmias is not always preceded by less severe signs of theophylline toxicity.

Elevated serum CK-MB levels have been associated with theophylline toxicity in the absence of cardiac disease. CK-MB levels have returned to normal following discontinuation of theophylline therapy.[Ref]

Metabolic

Metabolic side effects have included hypokalemia, hyperglycemia, respiratory alkalosis, hypophosphatemia, and hypomagnesemia, especially in the situation of acute overdosage. The magnitude of these abnormalities have been correlated with theophylline concentrations. Hypercalcemia has been reported in a patient with hyperthyroid disease with theophylline at therapeutic concentrations.[Ref]

In one group of patients with theophylline concentrations greater than 20 mcg/mL, hyperglycemia was present in approximately 50%, hypokalemia in 15%, and hypomagnesemia in 20%. Hyponatremia and hypophosphatemia were seen less frequently.[Ref]

Professional resources

Related treatment guides

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